TD52

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TD52 是 PP2A (CIP2A) 癌抑制剂的口服活性抑制剂。 TD52 是厄洛替尼衍生物，通过干扰 Elk1 与 CIP2A 启动子的结合来间接降低 CIP2A。

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.(In Vitro):TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2. TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt.(In Vivo):In female NCr athymic nude mice, TD52 (10 mg/kg/day; oral gavage) significantly inhibited MDA-MB-468 xenograft tumour size and tumour weight and decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours..

TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression.TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt. TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2. Apoptosis Analysis Cell Line:Three TNBC cell lines including HCC-1937, MDA-MB-231 and MDA-MB-468 cells Concentration:2, 4, 6, 8, 10 μM Incubation Time:48 hours Result:Showed anti-proliferative ability and induced differential apoptotic effects in these cell lines.Western Blot Analysis Cell Line:MDA-MB-231 cell Concentration:5 μM Incubation Time:48 hours Result:Had minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression.

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Animal Model:Female NCr athymic nude mice (5-7 weeks of age)Dosage:10 mg/kg Administration:Oral gavage; daily; for 52 days Result:Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.

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Apoptosis

Apoptosis

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1798328-24-1

360.41

C24H16N4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (277.46 mM)

N/A

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(-20℃)

With Ice Pack

≥ 2 years